1316099-70-3Relevant academic research and scientific papers
An access to chiral β-benzyl-γ-butyrolactones and its application to the synthesis of enantiopure (+)-secoisolariciresinol, (-)-secoisolariciresinol, and (-)-enterolactone
Allais, Florent,Pla, Thomas J. L.,Ducrot, Paul-Henri
experimental part, p. 1456 - 1464 (2011/06/17)
Both enantiomers of secoisolariciresinol and enantiopure (-)-enterolactone were synthesized through a highly stereoselective convergent synthesis. An Evans diastereoselective alkylation followed by a substrate-induced diastereoselective -alkylation of the newly formed optically active β-benzyl-γ- butyrolactone gave the β-β′ linkage of the target skeleton. The (S,S)- and (R,R)-enantiomers of secoisolariciresinol and (-)-enterolactone were obtained in 12-14% (11 steps) and 20% (7 steps) overall yield, respectively. Georg Thieme Verlag Stuttgart New York.
Design and optimization of potent and orally bioavailable tetrahydronaphthalene raf inhibitors
Gould, Alexandra E.,Adams, Ruth,Adhikari, Sharmila,Aertgeerts, Kathleen,Afroze, Roushan,Blackburn, Christopher,Calderwood, Emily F.,Chau, Ryan,Chouitar, Jouhara,Duffey, Matthew O.,England, Dylan B.,Farrer, Cheryl,Forsyth, Nancy,Garcia, Khristofer,Gaulin, Jeffery,Greenspan, Paul D.,Guo, Ribo,Harrison, Sean J.,Huang, Shih-Chung,Iartchouk, Natalia,Janowik, Dave,Kim, Mi-Sook,Kulkarni, Bheemashankar,Langston, Steven P.,Liu, Jane X.,Ma, Li-Ting,Menon, Saurabh,Mizutani, Hirotake,Paske, Erin,Renou, Christelle C.,Rezaei, Mansoureh,Rowland, R. Scott,Sintchak, Michael D.,Smith, Michael D.,Stroud, Stephen G.,Tregay, Ming,Tian, Yuan,Veiby, Ole P.,Vos, Tricia J.,Vyskocil, Stepan,Williams, Juliet,Xu, Tianlin,Yang, Johnny J.,Yano, Jason,Zeng, Hongbo,Zhang, Dong Mei,Zhang, Qin,Galvin, Katherine M.
, p. 1836 - 1846 (2011/05/30)
Inhibition of mutant B-Raf signaling, through either direct inhibition of the enzyme or inhibition of MEK, the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth. Very recently, treatment of B-Raf mutant melanoma patients with a selective B-Raf inhibitor has resulted in promising preliminary evidence of antitumor activity. This article describes the design and optimization of tetrahydronaphthalene-derived compounds as potent inhibitors of the Raf pathway in vitro and in vivo. These compounds possess good pharmacokinetic properties in rodents and inhibit B-Raf mutant tumor growth in mouse xenograft models.
